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Drug-carrying liposome modified by antimicrobial peptide and preparation method and application thereof

A technology of antimicrobial peptides and liposomes, applied in the field of biomedicine, can solve the problems of limited application, toxicity and death, hepatic hemorrhage, etc., and achieve the effects of alleviating drug resistance, high antibacterial activity, and reducing the number of bacteria

Active Publication Date: 2017-12-08
SICHUAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, when administered intravenously, it can cause hepatic hemorrhage and toxicity, while intraperitoneal administration requires a higher dose, which limits its further clinical application

Method used

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  • Drug-carrying liposome modified by antimicrobial peptide and preparation method and application thereof
  • Drug-carrying liposome modified by antimicrobial peptide and preparation method and application thereof
  • Drug-carrying liposome modified by antimicrobial peptide and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0064] Example 1 Synthesis of Antimicrobial Peptide DP7 and Cholesterol Conjugate (DP7-C)

[0065] Antimicrobial peptide DP7 and hydrophobic segment conjugates are made of figure 1Synthesized by the synthetic route shown. Wherein, the hydrophobic segment includes: cholesterol, cholic acid, palmitic acid, stearic acid, lauric acid and the like. 2-chlorotrityl chloride Resin, whose name is 2-chlorotrityl chloride resin; Fmoc-Rink Amide MBHA Resin, whose name is 4-(2',4'-dimethoxyphenyl-fluorenylmethoxycarbonyl- Aminomethyl)-phenoxyacetamido-methylbenzhydrylamine resin; Fmoc: fluorenylmethoxycarbonyl; pbf, tbu, Otbu, Trt, Boc are all protecting groups, the names are 2, 2, 4, 6 , 7-pentamethyldihydrobenzofuran-5-sulfonyl, tert-butyl, tert-butoxy, trityl, tert-butoxycarbonyl.

[0066] Concrete synthesis method is as follows:

[0067] 1. Resin swelling activation and deprotection:

[0068] Swelling: Weigh 1.0g Rink MBHA (4-(2′,4′-dimethoxyphenyl-fluorenylmethoxycarbonyl-aminome...

Embodiment 2

[0090] Preparation and characterization of liposomes modified by embodiment two DP7-C

[0091] 1. Liposome preparation and process optimization

[0092] Azithromycin-loaded liposomes (AZT-LPs) were prepared by thin film dispersion method.

[0093] The specific method is: accurately weigh 15.0mg soybean lecithin (SPC), 5.0mg cholesterol (Chol) (the mass ratio of lecithin and cholesterol is 3:1) and a certain amount of azithromycin are dissolved in 4mL chloroform solution; , in a 100mL round bottom flask, 37°C, 50 rpm, rotate under reduced pressure for 2h to evaporate the organic solvent to form a lipid film. Then, 4 mL of PBS solution was added to the flask, and the flask was rotated at 55°C to hydrate the lipid film for 40 min to prepare AZT-LPs. Afterwards, the above-mentioned liposome solution was sonicated with a probe at 85W power for 3 minutes (3 seconds of ultrasound, with an interval of 3 seconds), and then filtered with a 0.2 μm filter membrane to obtain a liposome s...

Embodiment 3

[0129] Embodiment three Liposome cytotoxicity detection of the present invention

[0130] Using human LO2 and HEK293 cells as model cells, Free AZT (250 μg / ml), AZT-LPs (250 μg / ml), D-LPs (250 μg / ml) and 1.25% AZT-D-LPs (62.5 μg AZT / ml+250μg DP7-C / ml), 2.5% AZT-D-LPs (125μg AZT / ml+250μg DP7-C / ml) and 5% AZT-D-LPs (250μg AZT / ml+250μgDP7-C / ml) Cell viability after 24 hours of liposome action. The cells in the logarithmic growth phase were collected, seeded in a 96-well plate at a density of 5×103 / well, and cultured in a cell culture incubator at 5% CO2, saturated humidity, and 37°C. After the cells adhered to the wall for 24 hours, 100 μl of Free AZT, AZT-LPs, D-LPs, and AZT-D-LPs solutions with different drug loadings were added to each well, and an equal volume of PBS was used as a negative control well. Concentration set up 3 parallel wells, and repeated 3 parallel experiments. After continuing to cultivate for 24 h, the mixture of drug and medium was removed, and then 20...

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Abstract

The invention belongs to the technical field of biological medicines, and particularly relates to drug-carrying liposome modified by antimicrobial peptide and a preparation method and application thereof. The liposome modified by the antimicrobial peptide is provided, the antimicrobial peptide is modified by a hydrophobic segment, the hydrophobic modified antimicrobial peptide is prepared by coupling the hydrophobic segment (or named as nitrogen tail end coupling a hydrophobic compound) at the nitrogen tail end, the amino acid sequence of the antimicrobial peptide is VQWRIRVAVIRK-NH2 beginning from the nitrogen tail end. The drug-carrying liposome is further provided, the drug-carrying liposome is obtained by loading antibiotics on the liposome. According to the liposome which are loaded with antibiotics, the antimicrobial peptide and the antibiotics are loaded into the liposome simultaneously, and good antibacterial activity in vivo, the immune regulation effect and good safety are achieved; and the liposome which are loaded with antibiotics is an ideal candidate drug for treating MRSA, and relieving of antibiotic resistance is facilitated, and new thoughts and strategies are provided for treating bacterial infection.

Description

technical field [0001] The invention belongs to the technical field of biomedicine, and in particular relates to a drug-loaded liposome modified with an antimicrobial peptide, a preparation method and application thereof. Background technique [0002] Globally, antibiotic resistance has seriously threatened human health. Infections caused by resistant bacteria such as MRSA (methicillin-resistant Staphylococcus aureus) and PRSP (penicillin-resistant Streptococcus pneumoniae) have a Clinical treatment presents enormous challenges. However, contrary to the rapid growth of drug-resistant bacteria, the development and production of new antibacterial drugs is very slow due to reasons such as poor water solubility, high toxicity, and high production costs. In order to find new antibacterial drugs or strategies with higher antibacterial activity and lower toxicity, researchers have tried to combine different antibiotics, combine antibiotics with other compounds, or use nanomaterial...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/69A61K47/64A61K45/00C07K7/08C07K1/10C07K1/107A61P31/04A61P31/10
CPCA61K45/00A61K9/127A61K31/7052A61K38/10A61K2300/00A61K39/39A61K9/107C07K7/08A61P31/04A61P31/10A01K2227/105A01K2267/0337A61K39/001135A61K39/001188A61K2039/53A61K2039/55561A61K38/00Y02P20/55A61K48/00Y02A50/30A61K47/6907A61K47/543A61K47/62A61K47/542A61K45/06C12N15/113C12N2310/14C12N2310/17
Inventor 杨莉何谷魏于全
Owner SICHUAN UNIV
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